克拉霉素日服一次缓释片的研制

目的：研制克拉霉素的凝胶合架型缓释片，筛选合适处方并考察体外释药特性。方法：以不同粘度规格羟丙基甲基纤维素为主要凝胶材料，体外释放速率为考察指标筛选处方。结果：药物释放速率符合Higuchi比方程，又体外释药速率受pH环境影响，在一定范围内受压片压力影响较小。经家犬体内药动学初步研究，测得相对生物利用度为94．2％。结论：本文研制的克拉霉素缓释片成型性好，体外释放曲线与国外市售制剂相似，具有较好的应用前景。

Development of Clarithromycin Sustained-Release Tablets

The purpose is to develop a sustained releas e dosage form of charithromycin(CLM) as hydrogel matrix tablet for using only once daily and evaluate its in vitro re lease characteristics. The formulations were screened acc ording to the re lease profile of reference tablet and the application of similarity factor was involved. HPMC was selected as the main gel materials. The release was p roperly characterized by the Higuchi equation which meant the diffusion erosion mechanism,influenced by pH of the media,the basket rotating speed and the tab let pressure exerted. After pharmacokinetics studies in dogs were carried out ,we got the similar pharmacokinetic parameters of self made tablets compared with reference tablets and the average relative bioavailability was 94 2%. The sustained release tablet of CLM had a similar profile of re lease in vitro to reference tablet and also showed similar behaviors in vivo ,thus having a good marketing prospect.